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Literature DB >> 21764310

Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.

Joseph B Kunicki¹, Mark N Petersen, Leslie D Alexander, Veronica C Ardi, Jeanette R McConnell, Shelli R McAlpine.

Abstract

Described are the syntheses of three sansalvamide A derivatives that contain biotinylated tags at individual positions around the macrocycle. The tagged derivatives indicated in protein pull-down assays that they bind to Hsp90 at the same binding site (N-Middle domain) as the San A-amide peptide. Further, these compounds inhibit binding between Hsp90 and multiple C-terminal client proteins. This interaction is unique to the San A analogs indicating they can be tuned for selectivity against Hsp90 client/co-chaperone proteins.

Entities: Chemical Disease Gene Species

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Year: 2011 PMID： 21764310 PMCID： PMC3155875 DOI： 10.1016/j.bmcl.2011.06.083

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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